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Phenothiazines and their Evolving Roles in Clinical Practice: A Narrative Review

The value of this class of medications should not be understated as they were the first antipsychotic medications developed. Still, the side effects of these medications should also be taken into consideration because they can pose a significant health risk. Phenothiazines have been used for decades to treat mental illnesses, including schizophrenia, mania in bipolar disorder, and psychosis. Additionally, they offer relief for physical illnesses such as migraines, hiccups, nausea, and vomiting in both adults and children. Still, further research is warranted to evaluate efficacy of phenothiazines in many disease states.

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 Never Say Dye: the Roots of Modern Psychiatric Medicines in Nineteenth-Century Fabric Colorings

Many modern psychiatric medicines share a single, and surprising, origin story. They stem from a 19th-century attempt to deal with the problem of malaria, and its unexpected consequence, the development of the synthetic fabric dye industry. To see how medicines as seemingly diverse as chlorpromazine, imipramine, clozapine, and diazepam evolved from this unlikely source, let us step back in time to the 1850s. At that point in time, malaria was taking a tremendous toll on the British effort to build and maintain an empire, and its devastation among the troops in the Crimean War was widely publicized.

Articles of Interest

First-Generation Antipsychotics: An Introduction

The phenothiazines are the largest chemical group, comprising more than 40 compounds... under three subtypes.

Phenothiazine: the seven lives of pharmacology's first lead structure

Rooted in the early days of organic dye chemistry, the phenothiazine structure and its derivatives have since held a prominent place in pharmacology and biomedicine. Initially used for histochemical stains of plasmodia by Paul Ehrlich, anthelmintic and antibiotic properties of phenothiazines were globally exploited in the 1930s and 1940s.

Phenothiazines and butyrophenones

Phenothiazines and butyrophenones are the antipsychotic (neuroleptic) agents. Commonly used agents are chlorpromazine, prochlorperazine, droperidol and haloperidol. Other unfamiliar agents include fluphenazine, Pericyazine, Pipothiazine and Trifluoperazine. If you think how you use these drugs in an aggressive patient you will understand their effects in overdose for a spectrum of CNS depression, orthostatic hypotension, anticholinergic effects and rarely dystonia.

Repurposing phenothiazines for cancer therapy: compromising membrane integrity in cancer cells

Phenothiazines belong to important antipsychotic drugs used for schizophrenia and bipolar disorder treatment. They demonstrate a broad spectrum of biological activities in mammalian cancer cells, as well as pathogenic bacteria and fungi with antipsychotic, antiemetic, antihistaminic, and anti-inflammatory properties. Beyond psychiatric use, phenothiazines may act as potential anticancer agents, targeting processes involved in tumor growth and metastasis.

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StatPearls

Phenothiazines are a class of first-generation heterocyclic anti-psychotic medications, which display antagonistic activity towards dopamine receptors and recently have been shown to have potential anti-neoplastic properties.